Exam 1 - Pharmacodynamics and kinetics Flashcards
How do Agonists bond to a receptor?
Ionic, Hydrogen, Van der Waals, Covalent
What is an Antagonist?
*How do they bind to a receptor?
Binds to the receptor, but does not activate the receptor
*Ionic, Hydrogen, Van der Waals, Covalent
What is Competitive Antagonism?
*Which way does the Dose Response Curve Shift?
Increasing amounts of this drug can progressively inhibit the agonist
*Right
What is Non-Competitive Antagonism?
The agonist cannot produce the agonist effect, even at high doses
What is a Partial Agonist?
Binds to the receptor at the agonist site and causes less agonistic response than the agonist
What is an Inverse Agonist?
*Name 6 Examples
They bind to the same site as the Agonist, but produce the opposite effect
*Propanolol, Metoprolol, Cetirizine, Loratadine, Prazosin, Narcan
What is Another name for Tolerance?
*Give 1 Drug and 1 Disease example
Tachyphylaxis
*Albuterol, Pheochromocytoma
What drugs would bind to the Lipid Bilayer?
Opiates, Benzo, BB, Catecholamines, NMBD
What drugs would bind to Intracellular Proteins?
Insulin, steroids, Milrinone
What drugs would bind to Circulating Proteins?
Anticoags
Name Vessel Rich Groups
*What % of body mass? % of CO?
Heart, Brain, Lungs, Kidney, Liver
* 10% Body mass; 75% CO
Name 6 Drugs Taken up by first pass through the lungs?
Lido, Propanolol, Meperidine, Fent, Sufent, Alfent
Where do Acidic drugs mostly bind?
Albumin
Where do Alkalotic Drugs mostly bind?
A1-Acid Glycoprotein
If 1/2 of the plasma proteins are lost, what happens to the free fraction of the drug?
DOUBLES!
* 2% free fraction becomes 4% free fraction
3 Examples of poor protein binding/lipophilic drugs
*Vd?
Thiopental, Valium, Prop
*Increased Vd
Example of Hydrophilic/highly protein bound drug?
*Vd?
Warfarin
*Small Vd
How are Paralytics Metabolized?
Hoffman Elimination and Ester Hydrolysis
Name the 3 Phase 1 Metabolism Methods
Oxidation, Reduction, Hydrolysis
Name the 1 Phase 2 Metabolism Method
Conjugation
What is Induction Activity Alteration?
*Ex
Increased the amount of enzyme, so enhances metabolism
*If you increased anti-coag metabolism, increased risk of bleeding
What is Inhibition Activity Alteration?
*Ex
Decreased the amount of enzyme, so slows metabolism leading to an increased drug toxic risk
*You inhibit enzyme that breaks down anti-coag, so increased clot risk
What is Flow limited Hepatic Clearance?
Rate proportional to Concentration - More drug = more clearance
What is Capacity Limited Hepatic Clearance?
Liver ability to metabolize is a limiting factor
What is the # for passive tubular reabsorption for Water soluble drugs [excreted in urine]
Almost 0
What is Elimination 1/2 Time
50% of drug from plasma after BOLUS dose
What is Elimination 1/2 Life
50% removed from the BODY
What is Context Sensitive Half-Time?
50% decrease after INFUSION d/c
Most drugs are _ acids and bases?
* Give example for each
Weak
*Acid - barb
*Base - LA and Opiates
Between Lipid Soluble and Water Soluble, which is Ionized?
Water soluble
*Lipid soluble is Non-ionized
Do we prefer to have the drug Ionized or Non-Ionized?
Non-Ionized
Formula for Weak Acids
Ph-PK
Formula for Weak Bases
PK-Ph
What is Potency vs Efficacy?
Potency - Concentration vs Response
Efficacy - Ability for a drug to produce a clinical effect
How to Calculate Therapeutic Index?
LD50/ED50
What is an Enantiomer: Optical Isomer?
Rotation of light in a solution
*Right - Dextrorotatory
*Left - Levorotatory
